ARTHOFLEX TABLETS (Each tablet contains Collagen Peptide Type II/Hyaluronic acid/Glucosamine 250mg/40mg/200mg)

Indications

• Symptomatic relief of mild to moderate osteoarthritis of the knee

Dosage

Children: Refer to the BNF for Children for

Adults: 200–400 mg daily, maximum 6.5 mg/kg per day, or 1250 mg once daily, or 1500 mg once daily dissolved in at least 250 mL of water; review treatment if no benefit after 2–3 months.

Mechanism of action

The mechanism of action of glucosamine in joint health is not entirely clear, but it is believed to involve several pathways. Glucosamine is a precursor for glycosaminoglycans, which are essential for cartilage integrity. It may also reduce inflammation by inhibiting interferon gamma and Nuclear factor kappa B subunit 65 (NF-κB p65), which could improve symptoms of arthritis and joint pain. Upon uptake by living cells, glucosamine reacts with ATP to form glucosamine-6-phosphate, further contributing to glycosaminoglycan synthesis.

Pharmacodynamics

Glucosamine is theorized to provide essential building blocks for the synthesis of glycosaminoglycans, potentially slowing the progression of osteoarthritis and alleviating joint pain. Although some studies have indicated modest improvements in joint pain and function among users, the overall evidence remains inconclusive. Glycosaminoglycans are critical for maintaining cartilage elasticity, strength, and flexibility, which are vital for joint health.

Pharmacokinetics

After oral administration, glucosamine is absorbed in the gastrointestinal tract and transported into the bloodstream, where it is metabolized into various forms, including glucosamine-6-phosphate. The exact pharmacokinetics, such as absorption rate and half-life, remain largely undefined, and much of the data is derived from animal studies. Further research is required to clarify its pharmacokinetic profiles in humans.

Adverse effects

• Constipation
• Diarrhoea
• Fatigue
• Gastrointestinal discomfort
• Headache
• Nausea
• Flushing
• Skin reactions

Interactions

• Glucosamine + warfarin: Severe (increases anticoagulant effect)
• Glucosamine + coumarins: Severe (increases anticoagulant effect)
• Glucosamine + acenocoumarol: Unknown (decreases anticoagulant effect)
• Glucosamine + coumarins: Unknown (decreases anticoagulant effect)

Precautions

• Asthma
• Impaired glucose tolerance
• Predisposition to cardiovascular disease

Pregnancy

Safety during pregnancy has not been established; consult with a healthcare provider.

Breast-feeding

Safety during breastfeeding has not been established; consult with a healthcare provider.

Storage

Store in a cool, dry place away from direct sunlight.

Formulations

• Alateris®
• Dolenio®
• Glusartel®

Indications

• Skin aging and wrinkle reduction
• Joint pain and osteoarthritis
• Tendon and ligament injuries
• Bone health
• Wound healing

Dosage

Children: Refer to specific product guidelines or consult a healthcare professional for appropriate dosing based on the indication and formulation used.

Adults: Refer to specific product guidelines or consult a healthcare professional for appropriate dosing based on the indication and formulation used.

Mechanism of action

Collagen exerts its effects primarily by providing the necessary amino acids, such as glycine, proline, and hydroxyproline, that are crucial for the synthesis of new collagen in the body. It is thought to stimulate fibroblast proliferation, which leads to increased collagen production and improved tissue repair. Additionally, collagen may enhance the hydration of the skin and improve its elasticity.

Pharmacodynamics

Collagen supplementation may promote the synthesis of new collagen and improve the integrity of the extracellular matrix. This can lead to improved skin hydration, elasticity, and the reduction of wrinkles. In joint health, collagen may help reduce inflammation and pain, contributing to improved mobility and function. The effects can vary based on the source of collagen (bovine, porcine, marine) and the form of administration (powder, liquid, capsules).

Pharmacokinetics

After oral administration, collagen peptides are absorbed in the gastrointestinal tract and enter the bloodstream. They can be transported to various tissues where they may be incorporated into the extracellular matrix. The half-life of collagen peptides is relatively short, and they are metabolized in the liver and other tissues. The bioavailability of collagen can vary based on the formulation and the presence of other dietary components.

Adverse effects

• Allergic reactions
• Skin rash
• Itching
• Gastrointestinal disturbances
• Nausea

Precautions

• Use with caution in individuals with fish allergies if derived from fish sources
• Monitor for allergic reactions

Pregnancy

Collagen is generally considered safe during pregnancy, but consult a healthcare professional before use.

Breast-feeding

Collagen is likely safe during breastfeeding, but consult a healthcare professional before use.

Storage

Store in a cool, dry place, away from direct sunlight. Keep out of reach of children.

Formulations

• Powder
• Capsules
• Liquid

Indications

• Osteoarthritis
• Dermal filler for aesthetic procedures
• Dry eye syndrome
• Surgical adjunct in ophthalmic procedures

Dosage

Children: Refer to specific product guidelines for dosing, as it varies by formulation and indication.

Adults: Refer to specific product guidelines for dosing, as it varies by formulation and indication.

Mechanism of action

Hyaluronic acid exerts its effects primarily through its ability to bind and retain water, thus contributing to tissue hydration and lubrication. In joints, it provides viscoelastic properties to synovial fluid, reducing friction and facilitating smooth movement. In dermal applications, it promotes skin moisture and elasticity by attracting water to the skin surface.

Pharmacodynamics

The pharmacodynamic properties of hyaluronic acid are attributed to its capacity to form a gel-like structure upon hydration, which enhances its mechanical and biological functions. In joint injections, it alleviates pain and improves function in patients with osteoarthritis by restoring the viscosity of synovial fluid. In cosmetic applications, its hydrophilic nature increases skin volume and smoothness, reducing the appearance of wrinkles.

Pharmacokinetics

Hyaluronic acid is administered via various routes, including intra-articular injections, topical formulations, and subdermal injections. After administration, it is distributed in the extracellular matrix, where it remains for varying durations depending on the formulation and site of application. The half-life can range from hours to days; however, once in the body, it is metabolized by hyaluronidases and other enzymes, with catabolites excreted primarily through urine.

Adverse effects

• Injection site reactions
• Allergic reactions
• Headache
• Dizziness

Precautions

• Use with caution in patients with a history of hypersensitivity to hyaluronic acid or any of its components
• Consider potential risks in patients with bleeding disorders or those on anticoagulant therapy

Pregnancy

Hyaluronic acid is generally considered safe for topical use during pregnancy, but systemic safety has not been fully established. Consult a healthcare provider before use.

Breast-feeding

Topical hyaluronic acid is considered safe for use during breastfeeding, but consult a healthcare provider for systemic use.

Storage

Store at room temperature, away from direct sunlight. Once opened, use as directed and do not freeze.

Formulations

• Injectable solutions
• Topical gels
• Ophthalmic solutions

Indications

• Hormone replacement therapy
• Diabetes management
• Metabolic disorders
• Cancer treatment
• Pain management
• Antimicrobial therapy

Dosage

Children: Paediatric dosing is also variable and should be determined based on specific guidelines for each peptide. Refer to paediatric dosing references for the appropriate dosages.

Adults: Dosage varies widely based on the specific peptide and condition being treated. Refer to specific product guidelines for appropriate dosing.

Mechanism of action

Peptides exert their effects by binding to specific receptors on the surface of target cells, which activates intracellular signaling pathways. This interaction can lead to various physiological responses, including modulation of enzyme activity, gene expression, and cellular metabolism.

Pharmacodynamics

The pharmacodynamic properties of peptides depend on their structure and the specific receptors they target. Peptides can exhibit high selectivity for their receptors, leading to minimal off-target effects. Dose-dependent responses are common, with many peptides showing a threshold effect below which no significant biological response is observed.

Pharmacokinetics

Peptides typically have a short half-life due to rapid degradation by proteolytic enzymes in the bloodstream. Their absorption can vary based on the route of administration, with oral bioavailability often being poor. For parenteral administration, factors such as the site of injection and formulation can influence their pharmacokinetic profile. Distribution is generally limited to the extracellular fluid, and elimination is primarily via renal pathways.

Pregnancy

Peptides should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Breast-feeding

Caution is advised when administering peptides during breastfeeding, as the effects on a nursing infant are not well studied.

Storage

Peptides should be stored at 2-8 degrees Celsius, protected from light and moisture. Once reconstituted, they should be used promptly or stored as recommended by the manufacturer.

Mechanism of action

The mechanism of action of glucosamine in joint health is unclear, however there are several possible mechanisms that contribute to its therapeutic effects. Because glucosamine is a precursor for glycosaminoglycans, and glycosaminoglycans are a major component of joint cartilage, glucosamine supplements may help to rebuild cartilage and treat the symptoms of arthritis. Some in vitro studies show evidence that glucosamine reduces inflammation via inhibition of interferon gamma and Nuclear factor kappa B subunit 65 (NF-κB p65), improving the symptoms of arthritis and joint pain. Clinical relevance is unknown at this time. When taken up by living cells, glucosamine reacts with ATP to form glucosamine-6-phosphate, the natural precursor of glycosaminoglycans (GAGs) that contain N-acetylglucosamine (keratan sulfate and Hyaluronan) and those that have N-acetylgalactosamine (heparan sulfate and chondroitin sulfate). These GAGs are polysaccharides composed of hexosamines and monosaccharides (e.g., galactose and glucuronic acid) arranged as a linear chain of repeating disaccharide units (such as the glucuronic acid and N-acetylgalactosamine-6-sulfate of chondroitin sulfate). With the exception of hyaluronan, GAGs do not exist alone in nature but are attached to specific "core" proteins, and the composite structures are called proteoglycans (protein-glycosaminoglycans). Both hyaluronan and many different kinds of proteoglycans (such as aggrecan, versican, and syndecan) are abundant throughout the body where they perform diverse functions.

Pharmacodynamics

The administration of glucosamine, in theory, provides a building block towards the synthesis of glycosaminoglycans, slowing the progression of osteoarthritis and relieving symptoms of joint pain. Studies to this date examining the efficacy of glucosamine sulfate have been inconclusive. Glycosaminoglycans contribute to joint cartilage elasticity, strength, and flexibility. A systematic review of various studies and guidelines determined that modest improvements were reported for joint pain and function in patients taking glucosamine. A consistent joint space narrowing was observed, but with an unclear clinical significance.